Cancer chemotherapy is a widely used treatment modality that has several limitations, including poor specificity, non-selective cytotoxicity, and systemic toxicity. Nanoparticles have emerged as promising drug delivery vehicles for cancer therapy due to their unique physicochemical properties and ability to improve drug efficacy and safety. Among various types of nanoparticles, gold nanoparticles have garnered significant attention due to their biocompatibility, ease of synthesis, and tunable size and surface chemistry. This review article summarizes the current state of knowledge on the use of gold nanoparticles for targeted and selective delivery of cancer chemotherapeutics. We discuss the various methods of synthesis and surface modification of gold nanoparticles for drug delivery, as well as the in vitro and in vivo studies demonstrating their efficacy and biocompatibility. Additionally, we highlight the mechanisms of gold nanoparticle-mediated chemotherapy delivery and the challenges and future directions in their development. Overall, this review underscores the promising role of gold nanoparticles as drug delivery vehicles for cancer therapy and highlights the potential for future clinical translation